fulvestrant
Ligand Summary
An estradiol derivative and estrogen receptor antagonist that is used for the treatment of estrogen receptor-positive, locally advanced or metastatic breast cancer.
UNII: 22X328QOC4
PubChem: 104741
Guide to Pharmacology: 1015
ChEMBL: CHEMBL1358
DrugCentral: 1255
LyCHI: D7416FK94ZF1
Target Activities
ESR1
Estrogen receptor
32 Activities
Items per page:
1 – 10 of 32
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.98 | |||||
IC50 | 10.22 | J Med Chem, (2017) 60:7:2790 | ||||
IC50 | 10.2 | J. Med. Chem., (2015) 58:20:8128 | ||||
IC50 | 9.6 | J Med Chem, (2021) 64:16.0:11841 | ||||
IC50 | 9.52 | J Med Chem, (2017) 60:14:6321 | ||||
IC50 | 9.49 | ACS Med Chem Lett, (2020) 11:6:1342 | ||||
EC50 | 9.4 | J. Med. Chem., (2015) 58:12:4888 | ||||
EC50 | 9.4 | Bioorg Med Chem Lett, (2019) 29:3:367 | ||||
IC50 | 9.33 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
IC50 | 9.11 | Bioorg Med Chem, (2019) 27:10:1952 | ||||
ESR2
Estrogen receptor beta
9 Activities
Items per page:
1 – 9 of 9
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 8.86 | |||||
Ki | 8.86 | J. Med. Chem., (2003) 46:8:1408 | ||||
IC50 | 8.42 | J. Nat. Prod., (2009) 72:11:1944 | ||||
IC50 | 8.15 | Bioorg. Med. Chem. Lett., (2000) 10:2:147 | ||||
IC50 | 8.08 | Bioorg. Med. Chem. Lett., (2005) 15:17:3912 | ||||
IC50 | 7.99 | Eur J Med Chem, (2020) 192:None:112191 | ||||
IC50 | 7.68 | J. Med. Chem., (2015) 58:12:4888 | ||||
IC50 | 7.36 | J. Med. Chem., (2007) 50:18:4471 | ||||
Ki | 8.74 | ANTAGONIST | ||||
EPHX2
Bifunctional epoxide hydrolase 2
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.22 | Bioorg. Med. Chem. Lett., (2013) 23:13:3818 | ||||
Ki | 7.58 | Bioorg. Med. Chem. Lett., (2013) 23:13:3818 | ||||
Ki | 7.59 | |||||
ESRRA
Steroid hormone receptor ERR1
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.7 | J. Med. Chem., (2013) 56:7:2779 | ||||
IC50 | 8.7 | |||||
GPER1
G-protein coupled estrogen receptor 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
- | 7 | |||||
PGR
Progesterone receptor
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.68 | J. Med. Chem., (2015) 58:20:8128 | ||||